SG10201403138WA - Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof and pharmaceutical use thereof - Google Patents

Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof and pharmaceutical use thereof

Info

Publication number
SG10201403138WA
SG10201403138WA SG10201403138WA SG10201403138WA SG10201403138WA SG 10201403138W A SG10201403138W A SG 10201403138WA SG 10201403138W A SG10201403138W A SG 10201403138WA SG 10201403138W A SG10201403138W A SG 10201403138WA SG 10201403138W A SG10201403138W A SG 10201403138WA
Authority
SG
Singapore
Prior art keywords
imidazo
pyrimidin
dihydro
derivatives
novel
Prior art date
Application number
SG10201403138WA
Inventor
Maurice Brollo
Annie Clauss
Ahmad Youssef El
Bruno Filoche-Romme
Frank Halley
Karl Andreas Karlsson
Gilbert Marciniak
Baptiste Ronan
Laurent Schio
Bertrand Vivet
Fabrice Viviani
André Zimmermann
Original Assignee
Sanofi Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from FR0903236A external-priority patent/FR2947550B1/en
Priority claimed from FR0957067A external-priority patent/FR2951173B1/en
Application filed by Sanofi Sa filed Critical Sanofi Sa
Publication of SG10201403138WA publication Critical patent/SG10201403138WA/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
SG10201403138WA 2009-07-02 2010-07-01 Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof and pharmaceutical use thereof SG10201403138WA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0903236A FR2947550B1 (en) 2009-07-02 2009-07-02 NOVEL 2,3-DIHYDRO-1H-IMIDAZO {1,2-A} PYRIMIDIN-5-ONE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB)
US24109709P 2009-09-10 2009-09-10
FR0957067A FR2951173B1 (en) 2009-10-09 2009-10-09 NOVEL 2,3-DIHYDRO-1H-IMIDAZO {1,2-A} PYRIMIDIN-5-ONE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE AS AKT PHOSPHORYLATION INHIBITORS (PKB)

Publications (1)

Publication Number Publication Date
SG10201403138WA true SG10201403138WA (en) 2014-08-28

Family

ID=43127464

Family Applications (2)

Application Number Title Priority Date Filing Date
SG10201403138WA SG10201403138WA (en) 2009-07-02 2010-07-01 Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof and pharmaceutical use thereof
SG2011097227A SG177421A1 (en) 2009-07-02 2010-07-01 Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof, and pharmaceutical use thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG2011097227A SG177421A1 (en) 2009-07-02 2010-07-01 Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof, and pharmaceutical use thereof

Country Status (25)

Country Link
US (1) US8828997B2 (en)
EP (1) EP2448939B1 (en)
JP (1) JP5663571B2 (en)
KR (1) KR101745028B1 (en)
CN (1) CN102482285B (en)
AR (1) AR077446A1 (en)
AU (1) AU2010267814B2 (en)
BR (1) BRPI1015949A2 (en)
CA (1) CA2767051C (en)
CY (1) CY1119442T1 (en)
DK (1) DK2448939T3 (en)
ES (1) ES2627428T3 (en)
HR (1) HRP20170827T1 (en)
HU (1) HUE034503T2 (en)
IL (1) IL217294A (en)
LT (1) LT2448939T (en)
MX (1) MX2012000097A (en)
PL (1) PL2448939T3 (en)
PT (1) PT2448939T (en)
RU (1) RU2554868C2 (en)
SG (2) SG10201403138WA (en)
SI (1) SI2448939T1 (en)
TW (1) TWI458730B (en)
UY (1) UY32753A (en)
WO (1) WO2011001112A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2969612B1 (en) * 2010-12-23 2013-02-08 Sanofi Aventis NOVEL 2,3-DIHYDRO-1H-IMIDAZO {1,2-A} PYRIMIDIN-5-ONE DERIVATIVES, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE
DK2655375T3 (en) * 2010-12-23 2015-03-09 Sanofi Sa PYRIMIDINON DERIVATIVES, PREPARATION AND PHARMACEUTICAL USE THEREOF
US9949979B2 (en) 2011-12-15 2018-04-24 Novartis Ag Use of inhibitors of the activity or function of PI3K
FR2992316A1 (en) * 2012-06-22 2013-12-27 Sanofi Sa PYRIMIDINONE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
FR2992314B1 (en) 2012-06-22 2015-10-16 Sanofi Sa NOVEL 2,3-DIHYDRO-1H-IMIDAZO {1,2-A} PYRIMIDIN-5-ONE AND 1,2,3,4-TETRAHYDRO-PYRIMIDO {1,2-A} PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, THEIR PREPARATION AND THEIR PHARMACEUTICAL USE
US10253028B2 (en) * 2015-01-23 2019-04-09 Glaxosmithkline Intellectual Property Development Limited Pyrazolo[3,4-D]pyrimidin derivative and its use for the treatment of leishmaniasis
AU2016307230B2 (en) * 2015-08-07 2019-02-21 Glaxosmithkline Intellectual Property Development Limited Compounds
JP2019086340A (en) * 2017-11-02 2019-06-06 シスメックス株式会社 Cell detection method and cell detection system
WO2022093820A1 (en) * 2020-10-28 2022-05-05 Genentech, Inc. Substituted morpholine compounds

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5888381A (en) * 1981-11-24 1983-05-26 Ube Ind Ltd Imidazopyrimidine compound
US20020077327A1 (en) * 1999-09-23 2002-06-20 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
MY125533A (en) * 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
US6977255B2 (en) 2000-01-24 2005-12-20 Kinacia Pty. Ltd. Therapeutic morpholino-substituted compounds
EP1184384A1 (en) * 2000-09-01 2002-03-06 Sanofi-Synthelabo 1-(Alkyl), 1-((heteroaryl)alkyl) and 1-((aryl)alkyl)-7-pyridin-4-ylimidazo(1,2a)pyrimidin-5(1H)-one derivatives
WO2002018386A1 (en) * 2000-09-01 2002-03-07 Sanofi-Synthelabo 2-PYRIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a]PYRIMIDIN-4-ONE AND 7-PYRIDINYL-2,3-DIHYDROIMIDAZO[1,2-a]PYRIMIDIN-5(1H)ONE DERIVATI VES
GB0119865D0 (en) 2001-08-14 2001-10-10 Cancer Res Campaign Tech DNA-PK inhibitors
EP1340761A1 (en) 2002-02-28 2003-09-03 Sanofi-Synthelabo Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives
ES2247398T3 (en) 2001-09-21 2006-03-01 Sanofi-Aventis DERIVATIVES OF 2-PIRIDINI9L-6,7,8,9-TETRAHYDROPIRIMIDO (1,2-A) PIRIMIDIN-4-ONA AND 7-PIRIDINIL-2,3-DIHYDROIMIDAZO (1,2-A) PIRIMIDIN-5 (1H) ONA SUBSTITUTED.
EP1340759A1 (en) * 2002-02-28 2003-09-03 Sanofi-Synthelabo 1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-(pyrimidin-4-yl)-imidazo[1,2-a]pyrimidin-5(1H)-one derivatives
ATE309247T1 (en) * 2002-02-28 2005-11-15 Sanofi Aventis HETEROARYL SUBSTITUTED 2-PYRIDINYL AND 2-PYRIMIDINYL-6,7,8,9-TETRAHYDROPYRIMIDO(1,2-A)PYRIMIDINE-4-ONE DERIVATIVES
US7598377B2 (en) 2002-08-16 2009-10-06 Astrazeneca Ab Inhibition of phosphoinositide 3-kinase β
CN1898243A (en) * 2003-12-23 2007-01-17 诺瓦提斯公司 Bicyclic heterocyclic p-38 kinase inhibitors
AR054438A1 (en) 2005-04-15 2007-06-27 Kudos Pharm Ltd DNA INHIBITORS -PK
WO2006126010A2 (en) * 2005-05-26 2006-11-30 Kudos Pharmaceuticals Limited Use of dna-pk inhibition to sensitise atm deficient cancers to dna-damaging cancer therapies
WO2008064244A2 (en) 2006-11-20 2008-05-29 The Trustees Of Columbia University In The City Of New York Phosphoinositide modulation for the treatment of neurodegenerative diseases
WO2008148074A2 (en) 2007-05-24 2008-12-04 Research Foundation Of State University Of New York Inhibitors of mtor and methods of treatment using same

Also Published As

Publication number Publication date
CN102482285B (en) 2015-07-15
AR077446A1 (en) 2011-08-31
AU2010267814A1 (en) 2012-02-16
EP2448939A1 (en) 2012-05-09
JP2012531462A (en) 2012-12-10
SG177421A1 (en) 2012-02-28
LT2448939T (en) 2017-06-12
CA2767051A1 (en) 2011-01-06
US20120142679A1 (en) 2012-06-07
RU2554868C2 (en) 2015-06-27
MX2012000097A (en) 2012-02-28
KR20120103552A (en) 2012-09-19
CN102482285A (en) 2012-05-30
TWI458730B (en) 2014-11-01
KR101745028B1 (en) 2017-06-08
TW201105672A (en) 2011-02-16
SI2448939T1 (en) 2017-06-30
UY32753A (en) 2011-01-31
AU2010267814B2 (en) 2015-07-16
IL217294A (en) 2015-07-30
JP5663571B2 (en) 2015-02-04
RU2012103460A (en) 2013-08-10
EP2448939B1 (en) 2017-03-01
CY1119442T1 (en) 2018-03-07
HRP20170827T1 (en) 2017-08-25
PL2448939T3 (en) 2017-08-31
PT2448939T (en) 2017-06-12
IL217294A0 (en) 2012-02-29
CA2767051C (en) 2017-08-22
DK2448939T3 (en) 2017-06-19
US8828997B2 (en) 2014-09-09
WO2011001112A1 (en) 2011-01-06
ES2627428T3 (en) 2017-07-28
BRPI1015949A2 (en) 2016-04-26
HUE034503T2 (en) 2018-02-28

Similar Documents

Publication Publication Date Title
HK1253364B (en) 1h-pyrazolo[3,4-b]pyridines and therapeutic uses thereof
IL215911A (en) 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives, pharmaceutical compositions comprising them and processes for their preparation and their use in the preparation of medicaments
SG10201403138WA (en) Novel 2,3-dihydro-1h-imidazo(1,2-a)pyrimidin-5-one derivatives, preparation thereof and pharmaceutical use thereof
SI2069342T1 (en) 2-ARYL-6-PHENYLIMIDAZO?á1,2-A?åPYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
IL213993A (en) 1,2,3,4-tetrahydropyrido[2,3-b]pyrazine-2-one derivatives and pharmaceutical compositions comprising them
IL200695A (en) Hydrooxazolo[3,2-a]pyrimidin-7-one derivatives and pharmaceutical compositions comprising the same
IL215644A (en) N-phenylsulfonyl-2-(1h-pyrrolo[2,3-b]pyridin-5-yloxy) benzamide derivatives and anti-cancer pharmaceutical compositions comprising them
HK1169388A1 (en) 6,7,8,9-tetrahydro-pyrimido1,2-a pyrimidin-4-one derivatives, their preparation and pharmaceutical use thereof 6789-12-a -4-
IL220432A (en) Thieno[2,3-b]pyridinedione derivatives and pharmaceutical compositions comprising the same
IL236170A0 (en) Novel 2,3-dihydro-1h-imidazo{1,2-a}pyrimidin-5-one and this1,2,3,4-tetrahydropyrimido{1,2-a} pyrimidin-6-one derivatives comprising a substituted morpholine, preparation thereof and pharmaceutical use thereof
IL206673A0 (en) Imidazo[1,2-a]pyridine-2-carboxamide derivatives, their preparation and their therapeutic application
IL212942A (en) Rifamycin derivatives, process for their preparation, pharmaceutical compositions comprising the same and uses thereof
SI1902054T1 (en) DERIVATIVES OF PYRIDO?á2,3-D?åPYRIMIDINE, THE PREPARATION THEREOF AND THE THERAPEUTIC APPLICATION OF THE SAME
IL223364A (en) 3,4-dihydropyrrolo[1,2-a] pyrazine-2,8 (1h)-dicarboxamide derivatives, preparation thereof and therapeutic use thereof
IL206671A0 (en) N-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
IL220448A (en) Substituted pyrido [2,3-d] pyrimidin-7 (8h)-ones and therapeutic uses thereof
IL206669A0 (en) 6-HETEROCYCLIC IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
EP2578586A4 (en) HEXAHYDROPYRROLO[3,4-b]PYRROLE DERIVATIVES, PREPARATION METHODS AND PHARMACEUTICAL USES THEREOF
IL206672A0 (en) N-HETEROCYCLIC-6-HETEROCYCLIC-IMIDAZO[1,2-a]PYRIDINE-2-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
IL215733A0 (en) 1-pyrazolo[4,3-c]isoquinoline derivatives, preparation thereof and therapeutic use thereof
IL206665A0 (en) 2-BENZOYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
IL206667A0 (en) 2-HETEROAROYLIMIDAZO[1,2-a]PYRIDINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF
IL213380A (en) Bicyclic derivatives of morphine-6-glucuronide, pharmaceutical compositions comprising them and use of same in the preparation of medicaments
HUP1000034A2 (en) Pyrido[1,2-a]pyrimidine derivatives and pharmaceutical preparations thereof having anti - mycobacterial activity